Abstract
A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral administration.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Animals
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacokinetics
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Calcium Channel Blockers / chemical synthesis*
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacokinetics
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Calcium Channels, N-Type / metabolism*
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Drug Discovery*
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Inhibitory Concentration 50
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Lactams / chemical synthesis*
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Lactams / chemistry
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Lactams / pharmacokinetics
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Molecular Structure
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Piperazines / chemistry
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Rats
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Solubility
Substances
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1-(6,6-bis(4-fluorophenyl)hexyl)-4-(3,4,5-trimethoxybenzyl)piperazine
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Biphenyl Compounds
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Calcium Channel Blockers
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Calcium Channels, N-Type
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Lactams
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Piperazines
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biphenyl